ULK1-IN-2

Research use only, not for human use.

ULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.

ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer).

ULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7.ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells.ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner.ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.Cell Proliferation Assay Cell Line:Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7 Concentration: 10 μM Incubation Time:24 h Result:Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively.Cell Autophagy Assay Cell Line:A549 cells Concentration:0, 2, 4, 8 μM Incubation Time:24 h Result:Blocked autophagy of A549 cells via inhibiting ULK.Western Blot Analysis Cell Line:A549 cells Concentration:0, 2, 4, 8 μM Incubation Time:24 h Result:Inhibited expression of ULK1 and p-ULK1ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.

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Autophagy

Autophagy

Autophagy | Apoptosis

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2497409-01-3

495.26

C19H16BrFN4O6

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (67.30 mM; Ultrasonic )

O(C)C1=C(OC)C=C(NC=2N=C(OC3=C(F)C=C(N(=O)=O)C=C3)C(Br)=CN2)C=C1OC

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(-20℃)

With Ice Pack

≥ 2 years